Author(s): Barbosa, Marília Imaculada Frazão ; Correa, Rodrigo de Souza ; Pozzi, Lucas Vinícius dos Santos ; Pavan, Fernando Rogério ; Leite, Clarice Queico Fujimura ; Ellena, Javier Alcides ; Machado, Sérgio de Paula ; Poelhsitz, Gustavo Von ; Batista, Alzir Azevedo
Date: 2016
Origin: Oasisbr
Subject(s): Mycobacterium tuberculosis; Ruthenium(II) complexes; Cytotoxicity; Metallodrugs; Hydroxypyridinecarboxylates
Three promising antimycobacterium tuberculosis ruthenium(II) complexes with the deprotonated ligands 2-hydroxynicotinic acid (2-OHnicH), 6-hydroxynicotinic acid (6-OHnicH) and 3-hydroxypicolinic acid (3-OHpicH) were synthesized and characterized. Structural analysis revealed three different coordination modes depending of the hydroxypyridinecarboxylate ligand. In the complex [Ru(2- OHnic)(dppb)(bipy)]PF6 (1), the 2-OHnic anion is coordinated by the O,O-chelating mode (via carboxylate group and phenolate oxygen), in the [Ru(6-OHnic)(dppb)(bipy)]PF6 (2) a O–O chelation by the carboxylate group is observed for the 6-OHnic ligand and for the complex [Ru(3-OHpic)(dppb)(bipy)]PF6 (3) a N,O-chelating mode (via carboxylate) occurs to the 3-OHpic anion. The compounds were evaluated for activity against Mycobacterium tuberculosis H37Rv ATCC 27294 using Resazurin Microtitre Assay (REMA) plate method and cytotoxicity in VERO CCL-81 cell line. All the synthesized compounds exhibited good antimycobacterial activity and a completely lack of cytotoxicity activity, indicating a good selectivity index.
